1Department
of Pharmaceutics, Government College of Pharmacy,
Bangalore, Pharmaceutical Chemistry Division, 2School
of Science and Humanities, Vellore Institute of
Technology, Vellore, Tamil Nadu, India
Purpose:
To evaluate the effect of formulation variables on the
bioadhesion and release properties of bioadhesive
cyproheptadine hydrochloride tablets.
Methods:
Screening of polymers
- hydroxypropyl methylcellulose, (HPMC), sodium carboxy
methyl cellulose (CMC), and Carbopol 974p and 934p - in
solution form were carried out by shear stress and
detachment force measurement,based on Taguchi model, in
order to determine their bioadhesion properties. Central
composite design (CCD) was applied to optimize the
combined effects of the polymers on release rate
constant (K), diffusion coefficient (n), regression
coefficient (R2) and detachment
force of a sustained release tablet formulation of
cyproheptadine hydrochloride containing also a prompt
dose of the drug.
Results:
The shear stress of 3 % solution of HPMC was greater
than that of an equivalent concentration of Carbopol
934P. The values of K, n, R2 and detachment
force for the optimized formulation (F0) were 0.269,
0.696, 0.964 and 0.066 Newton (N), respectively, and
showed good correlation with the predicted values, thus
confirming the practicability and validity of the model.
Conclusion:
Gastric retention time can be increased for
cyproheptadine hydrochloride by formulating it as a
bioadhesive tablet that enhances the retention of the
dosage form in the stomach and hence gastric absorption
of the drug.
Keywords:
Cyproheptadine hydrochloride, Bioadhesive core tablet,
Detachment force, Taguchi design, Central composite
design
